352 results about "Alkyne Compound" patented technology

The invention discloses a large optically anisotropic liquid crystal composition. The liquid crystal composition consists of a compound with a structural formula I, a compound with a structural formula II, a compound with a structural formula III and a compound with a structural formula IV; according to the liquid crystal composition, a series of liquid crystal materials with various structures are blended, and particularly a double-alkyne compound with extremely high optical anisotropy and maximum (delta)n of greater than 0.600 is adopted for the first time, so that the liquid crystal composition has great optical anisotropy; and meanwhile, the liquid crystal composition has high clearing point, appropriate dielectric anisotropy and acceptable rotary viscosity, and is particularly suitable for a liquid crystal display element LC-Lens and favorable for producing a thinner and more practical LC-Lens product by the device factory so as to obtain better visual experience and smooth 2D / 3D conversion effect.

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and / or eating disorders, particularly obesity and diabetes.

The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R<1 >and R<2 >have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and / or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

A composition and associated methods for chemical mechanical planarization (or other polishing) are described. The composition may comprise an abrasive and a dispersed hybrid organic / inorganic particle. The composition may further comprise an alkyne compound. Two different methods for chemical mechanical planarization are disclosed. In one method (Method A), the CMP slurry composition employed in the method comprises comprise an abrasive and a dispersed hybrid organic / inorganic particle. In another method (Method B), the CMP slurry composition employed in the method comprises comprise an abrasive and an alkyne compound. The composition may further comprise an oxidizing agent in which case the composition is particularly useful in conjunction with the associated methods (A and B) for metal CMP applications (e.g., tungsten CMP).

The disclosure includes methods for preparing organosilicon-containing 1,2,3-triazoles by reacting an organosilicon containing azide with an alkyne compound or an organosilicon containing alkyne with an azide compound under thermal reaction conditions.

The invention provides a one-pot method for synthesizing 1,2,3-triazole compounds, and belongs to the technical field of organic synthesis. According to the one-pot synthetic method for the 1,2,3-triazole compounds, nitrobenzene compounds and alkyne compounds serve as starting materials, and a plurality of the 1,2,3-triazole compounds are synthesized conveniently in a one-pot mode under the catalysis of copper. The 1,2,3-triazole compounds synthesized with the one-pot synthetic method are important intermediates for drug synthesis, and have very important application prospects in the fields including biomedicine, medicines and the like. Certain components are already widely used for clinics. The method adopts one-pot preparation, so that diazotization reaction is avoided, organic azides are not directly used, and the one-pot synthetic method for the 1,2,3-triazole compounds is high in safety, simple in operation, mild in conditions, low in cost and easy to use for industrial production and has good application prospects.

The present invention discloses a class of isocoumarin derivatives, which have the following general formula, wherein R is selected from hydrogen atom, C1-C10 alkyl, halogen, carbonyl, hydroxyl, nitrile, ester, alkoxy or trifluoromethoxyl, and E1 or E2 is selected from C1-C6 alkyl formate, phenyl or nitrile. The present invention further discloses a synthesis method of the isocoumarin derivatives. According to the present invention, divalent copper is adopted as a catalyst, a simple and easily-available o-halogenated benzoic acid and an alkyne compound are adopted as starting raw materials to synthesize an isocoumarin compound and derivatives thereof, and advantages of low cost, high yield, simple operation, easily-available raw materials, simple reaction equipment, easy industrial production, and the like are provided.

The present invention is directed to isotopically labeled alkyne derivative compounds, particularly 11C, 13C, 14C, 18F, 15O, 13N, 35S, 2H, and 3H labeled compounds. In particular, the present invention is directed to 11C, 13C, 14C, 18F, 15O, 13N, 35S, 2H, and 3H labeled heterocyclic alkynes and methods of their preparation. The present invention further includes a method of use of the 11C, 18F, 15O, or 13N labeled heterocyclic alkyne compounds as tracers in positron emission tomography (PET) imaging, particularly in the study of metabolic conditions in mammals, specifically conditions modulated by metabotropic glutamate receptors subtype 5 (mGluR5).

Alkyne compounds of formula I wherein A, B, W, X, Y, Z, R1, and R2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and / or eating disorders, particularly obesity and diabetes.

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula Iwherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

The invention discloses a preparation method of an N-containing graphdiyne material, wherein the preparation method comprises the steps: by using an N-containing six-membered heterocyclic compound anda metal alkyne compound as raw materials and ethanol as a solvent, carrying out ultrasonic reaction under the condition of ultrasonic frequency of 50-55 kHz, separating after the reaction is finished, washing a collected solid, and drying to obtain the N-containing graphdiyne material. The N-containing graphdiyne material is prepared by adopting an ultrasonic method, taking the N-containing six-membered heterocyclic compound and a metal alkyne compound as raw materials and taking ethanol as a solvent, nitrogen elements in the prepared N-containing graphdiyne material are distributed orderly,and the whole preparation method is simple to operate, mild in condition, green, environment-friendly and relatively low in equipment requirement; besides, experiments show that the N-containing graphdiyne material prepared by the method has excellent hydrogen evolution performance and energy storage performance, effectively promotes the application of the graphdiyne material in the fields of hydrogen evolution materials, supercapacitors, lithium ion battery negative electrode materials and the like, and has a wide industrial application prospect.

The invention discloses a synthesizing method of a 1,2,3-triazole compound of On-DNA during construction of a DNA coded compound storehouse. The method is divided into two types, wherein in one type of the method, an On-DNA alkyne compound is used as a substrate, in the presence of a Cu catalyst and an azide type reagent, the On-DNA alkyne compound reacts with micromolecule boric acid or a boric acid ester reagent to obtain a 1,4-disubstituted-1,2,3-triazole compound of the On-DNA; and in the other type of the method, an On-DNA azide compound is used as a substrate, in the presence of a metalNi catalyst or a metal Ru catalyst and a phosphine reagent, the On-DNA azide compound reacts with a micromolecule alkyne reagent to obtain a 1,5-disubstituted-1,2,3-triazole compound of On-DNA. According to the preparation method of the 1,2,3-triazole compound of the On-DNA, provided by the invention, the raw materials are easy to obtain, the reaction condition is mild, the production rate is high, the universality of the substrate is high, the selectivity of products is good, and the synthesizing method is suitable for synthesizing of a DNA coded compound storehouse using a porous plate.

The invention discloses preparation and application of an ordered mesoporous phenolic resin polymer silver-loaded catalyst. The preparation of the ordered mesoporous phenolic resin polymer silver-loaded catalyst is characterized in that the catalyst takes FDU mesoporous phenolic resin introduced with chloromethyl as a carrier, the carrier is connected with amido or sulfo adsorption immobilized silver ions in a covalent bond mode, and the silver ions are reduced in situ to generate a nulvalent-silver loaded type metal catalyst. Compared with the prior art, the preparation of the ordered mesoporous phenolic resin polymer silver-loaded catalyst has the advantages that catalytic activity is good, separation is facilitated, the catalytic yield is quite high during reaction under gentle conditions, moreover, the multi-phase catalyst is easy to recycle, can be reused and is pollution-free for the environment, preparation is simple, reaction conditions are gentle, and heavy metal pollution inheterogeneous catalytic reaction of carbon dioxide and a terminal alkyne compound is solved well.

The invention discloses 1,3-dihydro-2H-pyrrolidone compounds and a synthetic method thereof. A solvent and an alkali are added to a container containing substituted alpha-halogenated amide and a substituted alkyne compound, the mixture is stirred at the reaction temperature of 25-100 DEG C, a product is washed with water or a salt solution after the reaction and then extracted with an organic solvent, an extraction product is dried and distilled at reduced pressure to remove the solvent, a crude product is subjected to column chromatography separation, and the target product, namely, the 1,3-dihydro-2H-pyrrolidone compounds are obtained. The method has the advantages that no transition metal catalyst is used, the raw materials are cheap and available, reaction substrates are highly adaptable, reaction conditions are mild, regioselectivity is good, the yield is high, environmental protection is realized and the like, and has good industrial application prospect.

The present invention relates to a process which comprises efficiently proceeding a hydration reaction of an alkyne in aspects of turnover numbers of a catalyst, yield and speed to thereby industrially and advantageously produce the corresponding carbonyl compound. The present invention provides a process for producing a carbonyl compound, which comprises reacting an alkyne compound with water in the presence of a gold catalyst which is an organogold complex compound and acid in an organic solvent.

Alkyne compounds of formula I wherein A, B, W, X, Y, Z, R1, and R2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and / or eating disorders, particularly obesity and diabetes.

A method of preparing beta-chloroalkenyl sulfone compounds from sulfonates and alkynes is provided. The method includes directly synthesizing the beta-chloroalkenyl sulfone compounds from the sulfonates and the alkynes in a nitrogen or inert gas atmosphere by using an iron halogenide agent. The method adopts raw materials and the iron halogenide agent which are cheap, stable and easily available, and does not use ligands, acids, peroxides, microwave radiation, and other special reaction conditions. Pre-functionalization of a substrate is not needed. The method is mild in reaction conditions, simple in operation, short in reaction time and high in product selectivity, substrate applicability and yield, and has a potential application prospect in the fields of medicines, organic synthesis intermediates, and the like.

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula Iwherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

The invention relates to a heterocycle 1, 4-disubstituted-1, 2, 3-triazole compound and a synthesizing method thereof. A halomethylated heterocycle compound and sodium azide and terminal alkyne compounds generate 1, 3-dipolar cycloaddition reaction through simple process and mild condition under the action of a phase transfer catalyst to synthesize the heterocycle 1, 4-disubstituted-1, 2, 3-triazole derivative with high selectivity and high yield. The compound is an important medicinal intermediate, and simultaneously has potential in pesticide, fine chemistry industry and other fields. In the formula of the compound, heterocycle-1, 4 is a nitrogen heterocyclic ring: imidazole and derivatives thereof, benzoglioxaline and derivatives thereof, benzotriazol, indole and derivatives thereof, carbazole and derivatives thereof; Y is H or F, n is equal to between 1 and 8; and r presents Ar, Alk and Bn.

The invention belongs to the field of catalysts, and in particular relates to a palladium-free, amine-free and ligand-free copper catalyst system. The catalyst system can catalyze a Sonogashira reaction to prepare alkyne compounds. The catalyst system comprises cupric salt, potassium carbonate and a solvent dimethyl sulfoxide, wherein the molar ratio of the cupric salt to the potassium carbonate is 1:20-40; and the cupric salt is one or the mixture of more than one of copper acetate, copper acetylacetonate, copper trifluoromethanesulfonate and copper sulfate. In the catalyst system, noble metal is replaced by the stable cupric salt, so that the catalyst system is economic, cheap and non-toxic; for a substrate with poor activity, the catalyst system is added with TBAB to promote the reaction remarkably; and the catalyst system is suitable for large-scale application and industrialized production.

The invention belongs to the technical field of organic synthesis chemistry and particularly relates to a preparation method of an N-vinyl-1,2,3-triazole compound. The preparation method comprises thefollowing steps: firstly, adding a terminal alkyne compound 1, a compound 2 and a nucleophilic reagent Nu into a solvent containing triethylamine; then, adding a Pd / Cu catalyst into a reaction system, heating for reaction under the protection of argon, where the reaction ends after a substrate disappears; secondly, carrying out vacuum distillation on reaction liquid obtained in the first step, removing an organic solvent, and eluting the obtained liquid to obtain the N-vinyl-1,2,3-triazole compound. The N-vinyl-1,2,3-triazole is obtained by adopting a method for in situ generation of 2-azidopropylene and derivatives thereof. The method has the advantages of extremely-simple operation, simple and easily-obtained substrates and catalysts, excellent universality of the substrates, good tolerance of functional groups and insensitivity to the ambient atmosphere and uniform and excellent yield.

The invention discloses a method for synthesizing a palladium catalyst by utilizing alkyne compounds and relates to a synthesizing method of a palladium catalyst. The method comprises the following steps: adding a Pd precursor in a solvent; then adding a carrier and an alkyne compound sequentially to have a reaction; at the end of the reaction, separating, washing and drying the obtained product, thus obtaining the palladium catalyst, wherein the obtained palladium catalyst is a polymerization-alkyne-loaded palladium catalyst. Alkyne is subjected to polymerization reaction in the presence of Pd; meanwhile, Pd also can be coordinated with the generated polymer, thereby obtaining a polymerization-alkyne-immobilized Pd catalyst. Meanwhile, in order to enable the obtained catalyst to be more practical, the catalyst can be adsorbed on the carrier in situ as long as a proper amount of carrier is added directly in the reaction solution, and further an immobilized catalyst is obtained. The obtained product is easy to separate and process, and is stable to air and water. The method is simple and feasible; raw materials are easily available and are easy to synthesize in a large scale. Meanwhile, the catalyst shows favorable catalytic activity and has a wide actual application prospect.

The invention discloses a synthesis method of a 1, 5-benzodiazepine derivative, which is obtained by an intermolecular amination / cyclization tandem reaction process of an o-phenylene diamine compound and an alkyne compound in the presence of a catalyst. The method of the invention is characterized in that the alkyne is used as a starting material for the first time and utilization ratio of reacted atoms is 100%. The method further has good general adaptability for various substituent groups.

The invention discloses a hyperbranched polythioamide compound as well as a preparation method and application thereof. The preparation method of the hyperbranched polythioamide compound comprises thefollowing steps: in the presence of nitrogen or an inert gas, by taking an organic solvent I as a reaction medium, uniformly mixing a polyalkyne compound, a polyamine compound and elemental sulfur, carrying out a polymerization reaction at 80-120 DEG C, and carrying out purification, so as to obtain the hyperbranched polythioamide compound. The preparation method disclosed by the invention is easy in reaction raw material obtaining, gentle in polymerization condition, simple in process and high in polymerization efficiency. The hyperbranched polythioamide compound is applied to fields of goldion adsorption and photoelectric devices.

The invention discloses a compound containing trifluoromethylthio group and a preparation method thereof. The invention discloses a compound 7, compound 9 or compound 11 containing trifluoromethylthio group. The invention provides a preparation method of the compound 7, 9 or 11, which comprises the following steps: in an organic solvent, carrying out substitution reaction on a compound 1 and a beta-eleostearate compound 6 in the presence of an alkali to obtain the compound 7; in an organic solvent, carrying out substitution reaction on the compound 1 and an aldehyde or ketone compound 8 in the presence of a catalyst and an additive to obtain the compound 9; and under the gas protection, carrying out substitution reaction on the compound 1, cuprous iodide and an alkyne compound 10 in an organic solvent in the presence of an alkali to obtain the compound 11. The preparation method of the compound 7, 9 or 11containing trifluoromethylthio group has the advantages of mild reaction conditions, high conversion rate, high yield and low production cost, and is suitable for industrial production.

The invention relates to a new photocatalytic fixed-point deuteration method for carbon-carbon unsaturated bonds. The method is characterized in that an olefin or alkyne compound and a deuterium source undergoes a deuteration reaction under the catalysis of a light source and a photocatalyst to obtain a deuterated product, wherein the deuterium source is deuterated water, deuterated alcohol or deuterated acid, and the reaction temperature is between room temperature and 80 DEG C. The fixed-point deuteration reaction of the olefin or alkyne compound is realized under the photocatalysis action of the photocatalyst with environmentally-friendly and cheap deuterated water or a deuteration reagent as a deuterium source to substitute deuterium gas. Compared with traditional deuteration reactions, the method has a higher selectivity, milder reaction conditions and higher economical suitability, and is suitable for large-scale deuterated chemical substance production.

The invention relates to modified silicon-containing aryne resin. A preparing method of the modified silicon-containing aryne resin includes the following steps: (1) preparing silicon-containing aryne polymer, (2) preparing benzoxazine compound, (3) preparing propargyl ether compound, and (4) preparing the modified silicon-containing aryne resin, mixing 50-90 parts by weight of the silicon-containing aryne polymer obtained through the step (1), 5-25 parts by weight of the benzoxazine compound obtained through the step (2) and 5-25 parts by weight of the propargyl ether compound obtained through the step (3), and leading the mixture to be stirred for reacting in a reactor comprising a stirrer, a thermometer and a reflux condensing pipe with inert gases to obtain the modified silicon-containing aryne resin. The oxazine and alkyne compound modified silicon-containing aryne resin and the preparing method of the modified silicon-containing aryne resin have the advantages that the modified silicon-containing aryne resin can be dissolved in many common solvents, is low in softening point and melting resin viscosity, and can generate solidifying reaction under heat, irradiation and even light effect. Resin condensates are good in heat resistance and can be well bonded with reinforcing fiber, and compound materials of the modified silicon-containing aryne resin have good mechanical performance and heat resistance.

A hydrogenation promoter of the present invention is produced by reacting an alkyne compound or an alkene compound, a palladium compound represented by a general formula Pd(II)XjLk (where L represents a monodentate ligand or a polydendate ligand other than a phosphorus-containing ligand (when two or more Ls are present in the compound, the Ls may be the same or different), X represents an anionic group, j represents a value determined according to the valence of X so that Xj has a valence of −2 as a whole, and k represents an integer in the range of 0 to 4), and a base in an organic solvent. Specifically, The hydrogenation promoter of the invention includes palladium nanoparticles containing the alkyne compound or the alkene compound as an agglomeration-preventing agent.